Premium
High‐ and Low‐Affinity Binding Components for [ 3 H]Imipramine in Rat Cerebral Cortex
Author(s) -
Conway P. G.,
Brunswick D. J.
Publication year - 1985
Publication title -
journal of neurochemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.75
H-Index - 229
eISSN - 1471-4159
pISSN - 0022-3042
DOI - 10.1111/j.1471-4159.1985.tb05494.x
Subject(s) - imipramine , dissociation (chemistry) , cerebral cortex , dissociation constant , membrane , chemistry , binding site , biophysics , endocrinology , biochemistry , receptor , biology , medicine , alternative medicine , pathology
The present study demonstrates that [ 3 H]imipramine binds to both high‐ and low‐affinity imip‐ramine binding components on membranes prepared from rat cerebral cortex. Scatchard and computer analyses of saturation experiments using a wide range of [ 3 H]imipramine concentrations (0.5 n M‐ 50 n M ) revealed the presence of two binding components. Inhibition experiments in which membranes were incubated with [ 3 H]imipramine and various concentrations of unlabelled imipramine gave shallow inhibition curves with a Hill coefficient of 0.60 ± 0.04. When dissociation rates of imipramine were studied, biphasic dissociation curves were obtained with apparent half‐times of dissociation of 2.5 ± 0.4 min and 18.5 ± 2.5 min. Thus analysis of saturation, competition, and dissociation experiments indicate that [ 3 H]imipramine binds to low as well as high‐affinity binding sites in rat cortex.